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US4250117A - 4-Hydroxy-4-methyl-cyclohexen-2-one-1 - Google Patents

4-Hydroxy-4-methyl-cyclohexen-2-one-1 Download PDF

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Publication number
US4250117A
US4250117A US05/932,076 US93207678A US4250117A US 4250117 A US4250117 A US 4250117A US 93207678 A US93207678 A US 93207678A US 4250117 A US4250117 A US 4250117A
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United States
Prior art keywords
compound
methyl
hydroxy
mixture
cyclohexen
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Expired - Lifetime
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US05/932,076
Inventor
Katsuhiro Takahashi
Shigeru Muraki
Toshio Yoshida
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Takasago International Corp
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Takasago Perfumery Industry Co
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Assigned to TAKASAGO PERFUMERY CO., LTD reassignment TAKASAGO PERFUMERY CO., LTD ASSIGNMENT OF ASSIGNORS INTEREST. Assignors: MURAKI,SHIGERU, TAKAHASHI, KATSUHIRO, YOSHIDA, TOSHIO
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Classifications

    • CCHEMISTRY; METALLURGY
    • C11ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
    • C11BPRODUCING, e.g. BY PRESSING RAW MATERIALS OR BY EXTRACTION FROM WASTE MATERIALS, REFINING OR PRESERVING FATS, FATTY SUBSTANCES, e.g. LANOLIN, FATTY OILS OR WAXES; ESSENTIAL OILS; PERFUMES
    • C11B9/00Essential oils; Perfumes
    • C11B9/0026Essential oils; Perfumes compounds containing an alicyclic ring not condensed with another ring
    • C11B9/0034Essential oils; Perfumes compounds containing an alicyclic ring not condensed with another ring the ring containing six carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/62Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by hydrogenation of carbon-to-carbon double or triple bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/703Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
    • C07C49/713Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups a keto group being part of a six-membered ring

Definitions

  • This invention relates to a novel compound useful as a perfume component. More specifically, this invention relates to 4-hydroxy-4-methyl-cyclohexan-2-one-1 useful as a perfume component.
  • This invention provides 4-hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I): ##STR2##
  • Compound (I) 4-Hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I) above [hereinafter "Compound (I)" of this invention] neat is a substance having a phenol-like or cattle pen-like odor. However, when Compound (I) is diluted to a great extent, it imparts a fragrance organoleptically felt to be warm and giving a sweet impression. It has been found that when Compound (I) is blended with other perfume components in a perfume composition in an amount of about 2 to about 15 ppm, preferably 5 to 10 ppm, favorable results which one can readily organoleptically recognize are obtained.
  • Compound (I) of this invention when Compound (I) of this invention is mixed with various synthetic essential oils such as petigrain oil, lavandine oil, lavender oil, orange oil, lemon oil, bergamot oil, peppermint oil, spearmint oil, etc., the naturalness of the odor of the blend can be markedly increased. Further, when Compound (I) is blended with other perfume components for perfumes, soaps, foods and the like, it can also impart a fragrance organoleptically felt to be warm and giving a sweet impression.
  • synthetic essential oils such as petigrain oil, lavandine oil, lavender oil, orange oil, lemon oil, bergamot oil, peppermint oil, spearmint oil, etc.
  • N-(p-methylphenyl)-hydroxylamine (III) can be obtained from p-nitrotoluene (II) using the nitrobenzene reduction method as described in, for example, H. Gilman, Organic Syntheses, Collective Vol. 1, 2nd Ed., pp 445-447 (1961), John Wiley & Sons, Inc., N.Y., or Y. Ogata et al, J. Am. Chem. Soc., 86, pp 3854-3858 (1964).
  • the concentrate thus obtained is purified with a diethyl ether-benzene mixture on a silica gel chromatographic column to obtain pure p-toluquinol (IV) having a melting point of 76° to 78° C.
  • Compound (IV) is then partially hydrogenated in ethyl alcohol with a 5% Pd/C catalyst at room temperature (e.g., about 20°-30° C.) under a hydrogen pressure of one atm. to obtain Compound (I) having a boiling point of 101.5° to 109.5° C./2 mmHg.
  • step (i) above 50 g of p-tolylhydroxyl amine obtained in step (i) above was added incrementally to 1 l of a 5% sulfuric acid aqueous solution cooled to 0° C. using an ice-NaCl bath over a period of about 15 minutes while slowly stirring the mixture. After completion of the addition, the ice-NaCl bath was removed, and the mixture was slowly stirred at room temperature (i.e., about 20°-30° C.) for 12 hours. The reaction mixture was filtered, and the filtrate was extracted with 1 l of chloroform. The chloroform was distilled off from the extract to obtain 300 g of a concentrate.
  • This concentrate was then chromatographed on a silica gel column, and eluted with a diethyl ether-benzene (1:1 by volume) mixture to obtain a fraction.
  • the thus-obtained fraction was concentrated to obtain 15 g of p-toluquinol.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Wood Science & Technology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Fats And Perfumes (AREA)
  • Cosmetics (AREA)

Abstract

4-Hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I): ##STR1##

Description

BACKGROUND OF THE INVENTION
This invention relates to a novel compound useful as a perfume component. More specifically, this invention relates to 4-hydroxy-4-methyl-cyclohexan-2-one-1 useful as a perfume component.
SUMMARY OF THE INVENTION
This invention provides 4-hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I): ##STR2##
DETAILED DESCRIPTION OF THE INVENTION
4-Hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I) above [hereinafter "Compound (I)" of this invention] neat is a substance having a phenol-like or cattle pen-like odor. However, when Compound (I) is diluted to a great extent, it imparts a fragrance organoleptically felt to be warm and giving a sweet impression. It has been found that when Compound (I) is blended with other perfume components in a perfume composition in an amount of about 2 to about 15 ppm, preferably 5 to 10 ppm, favorable results which one can readily organoleptically recognize are obtained. For example, when Compound (I) of this invention is mixed with various synthetic essential oils such as petigrain oil, lavandine oil, lavender oil, orange oil, lemon oil, bergamot oil, peppermint oil, spearmint oil, etc., the naturalness of the odor of the blend can be markedly increased. Further, when Compound (I) is blended with other perfume components for perfumes, soaps, foods and the like, it can also impart a fragrance organoleptically felt to be warm and giving a sweet impression.
Compound (I) of this invention can be, for example, prepared in accordance with the following reaction schematic: ##STR3##
In the above-described reaction schematic, N-(p-methylphenyl)-hydroxylamine (III) can be obtained from p-nitrotoluene (II) using the nitrobenzene reduction method as described in, for example, H. Gilman, Organic Syntheses, Collective Vol. 1, 2nd Ed., pp 445-447 (1961), John Wiley & Sons, Inc., N.Y., or Y. Ogata et al, J. Am. Chem. Soc., 86, pp 3854-3858 (1964). More specifically, for example, 1 mole of p-nitrotoluene (II) is reduced with 2 moles of zinc dust in a solution of 1 mole of ammonium chloride, and the resulting product is recrystallized from a benzene-petroleum ether mixture to obtain Compound (III) having a melting point of 94° C. Subsequently, Compound (III) is treated with a 5% sulfuric acid aqueous solution while cooling to approximately 0° C., e.g., in accordance with the method described in S. Goodwin et al, J. Am. Chem. Soc., 79, pp 179-185 (1957). After extracting the resulting product with chloroform, the concentrate thus obtained is purified with a diethyl ether-benzene mixture on a silica gel chromatographic column to obtain pure p-toluquinol (IV) having a melting point of 76° to 78° C. Compound (IV) is then partially hydrogenated in ethyl alcohol with a 5% Pd/C catalyst at room temperature (e.g., about 20°-30° C.) under a hydrogen pressure of one atm. to obtain Compound (I) having a boiling point of 101.5° to 109.5° C./2 mmHg.
This invention is explained in more detail with reference to the following examples. Unless otherwise indicated herein, all parts, percents, ratios and the like are by weight.
The following Formulation Examples are given to illustrate representative examples of perfumes in which Compound (I) of this invention can be used. These Formulation Examples should not be construed as limiting the use of Compound (I) of this invention, however.
FORMULATION EXAMPLE 1
0.01 g (10 ppm) of Compound (I) of this invention was added to 1000 g of synthetic lavandine oil having the formulation shown in Table 1 below.
              TABLE 1                                                     
______________________________________                                    
(Formulation of Synthetic Lavandine Oil)                                  
                            Weight                                        
Components                  (g)                                           
______________________________________                                    
Cineole                     200                                           
Ocimene                     100                                           
Camphor                     90                                            
Aldehyde C.sub.13           90                                            
(5,2,1,0)Tricyclo-3-decen-8-yl Acetate                                    
                            70                                            
Bornyl Acetate              50                                            
iso-Pulegyl Acetate         50                                            
Borneol                     42                                            
iso-Dihydro-lavandulyl Aldehyde                                           
                            42                                            
Octyl iso-Butyrate          40                                            
Ethyl Amyl Ketone           30                                            
Heptyl Aldehyde*            28                                            
Hexyl Aldehyde*             14                                            
Octyl Aldehyde*             14                                            
Cuminaldehyde*              14                                            
Linalyl iso-Valerate        28                                            
Linalyl iso-Butyrate        8                                             
Linalool Oxide              8                                             
n-Octyl Alcohol             14                                            
n-Hexyl Alcohol             8                                             
n-Octyl Acetate             8                                             
n-Hexyl Acetate             14                                            
Dihydro Terpineol           14                                            
Geraniol                    8                                             
n-Amyl Alcohol              6                                             
Methyl Chrysanthemate       10                                            
Total:                      1000                                          
______________________________________                                    
 *1% in benzyl benzoate.                                                  
As a result of an organoleptic evaluation using 10 panelists, all of the 10 panelists recognized that the naturalness of the resulting perfume composition was markedly improved as compared with the same perfume composition to which Compound (I) of this invention was not added.
FORMULATION EXAMPLE 2
0.005 g (5 ppm) of Compound (I) of this invention was added to 1000 g of synthetic peppermint oil having the formulation shown in Table 2 below.
              TABLE 2                                                     
______________________________________                                    
(Formulation of Synthetic Peppermint Oil)                                 
                    Weight                                                
Components          (g)                                                   
______________________________________                                    
Menthol             474                                                   
Menthone            250                                                   
1,8-Cineole         65                                                    
Menthyl Acetate     36                                                    
iso-Menthone        35                                                    
Terpinene-4-ol      32                                                    
α-Terpineol   20                                                    
Menthofuran         17                                                    
l-Limonene          15                                                    
β-Pinene       12                                                    
α-Pinene      9                                                     
Piperitone          5                                                     
Caryophyllene       5                                                     
Linalool            4                                                     
3-Octanol           3                                                     
p-Cymene            3                                                     
β-Myrcene      3                                                     
1-Octen-3-ol        2                                                     
iso-Valeraldehyde   2                                                     
cis-Jasmone         2                                                     
iso-Amyl Alcohol    0.6                                                   
cis-3-Hexenol       0.5                                                   
Mint Lactone        0.5                                                   
1-Octen-3-yl Isovalerate                                                  
                    0.4                                                   
n-Hexyl Aldehyde    0.4                                                   
t-2-Hexenol         0.4                                                   
Eugenol             0.4                                                   
n-Hexanol           0.3                                                   
t-Jasmone           0.3                                                   
3-Octyl Acetate     0.3                                                   
1-Octen-3-yl Acetate                                                      
                    0.3                                                   
Pulegone            0.3                                                   
iso-Valeric Acid    0.3                                                   
cis-3-Hexenyl Acetate                                                     
                    0.2                                                   
Citronellyl Acetate 0.2                                                   
Geranyl Acetone     0.2                                                   
Carbacrol           0.2                                                   
2-Methylpropanol    0.1                                                   
Thymol              0.1                                                   
Total:              1000                                                  
______________________________________                                    
As a result of an organoleptic evaluation using 10 panelists, all of the 10 panelists recognized that the naturalness of the resulting perfume composition was markedly improved as compared with the same perfume composition to which Compound (I) of this invention was not added.
EXAMPLE (i) Preparation of p-Tolylhydroxyl Amine
281 g (2.05 moles) of p-nitrotoluene, 125 g (2.35 moles) of ammonium chloride and 4 l of water were charged into a 10-l reaction flask. 310 g (4.74 moles) of zinc dust was added thereto at room temperature (i.e., about 20°-30° C.) over a period of 15 minutes while stirring the mixture, and the mixture was stirred for an additional 30 minutes. In this case, the temperature of the reaction system increased to 65° to 70° C. with stirring. Thereafter, the reaction mixture was filtered, and the filtrate was saturated with sodium chloride. The filtrate was allowed to stand in a cool place for 24 hours. The precipitated crystals were filtered, and recrystallized from 1 l of a benzene-petroleum ether (1:1 by volume) mixture to obtain 50 g of p-tolylhydroxyl amine.
(ii) Preparation of p-Toluquinol
50 g of p-tolylhydroxyl amine obtained in step (i) above was added incrementally to 1 l of a 5% sulfuric acid aqueous solution cooled to 0° C. using an ice-NaCl bath over a period of about 15 minutes while slowly stirring the mixture. After completion of the addition, the ice-NaCl bath was removed, and the mixture was slowly stirred at room temperature (i.e., about 20°-30° C.) for 12 hours. The reaction mixture was filtered, and the filtrate was extracted with 1 l of chloroform. The chloroform was distilled off from the extract to obtain 300 g of a concentrate. This concentrate was then chromatographed on a silica gel column, and eluted with a diethyl ether-benzene (1:1 by volume) mixture to obtain a fraction. The thus-obtained fraction was concentrated to obtain 15 g of p-toluquinol.
(iii) Preparation of 4-Hydroxy-4-methyl-cyclohexen-2-one-1
50 g of p-toluquinol obtained in step (ii) above was dissolved in 50 g of ethyl alcohol. The mixture was hydrogenated with 5% palladium-on-carbon as a catalyst while shaking the mixture at room temperature under a hydrogen pressure of one atm. When 80% of the amount of hydrogen theoretically necessary for hydrogenation to an extent of 0.5 mole was absorbed, the reaction was stopped. After filtering off the catalyst, the residue was distilled under reduced pressure to obtain 47 g of a fraction having a boiling point of 101.5°-109.5° C./2 mmHg. This fraction was a colorless liquid and had the following characteristics.
______________________________________                                    
Specific Gravity d.sub.20.sup.20 :                                        
               1.0842                                                     
Refractive Index n.sub.D.sup.20 :                                         
               1.5163                                                     
Mass Spectral Analysis:                                                   
               M.sup.⊕ 126 111 (M--CH.sub.3)                          
Infrared Analysis:                                                        
               ν cm.sup.-1 3400 (--OH), 1675 (C═O)                 
Nuclear Magnetic Resonance Analysis:                                      
             δ ppm                                                  
                   1.4     (3H, s) H.sub.7                                
                   1.9-2.7 (4H, m) H.sub.5, H.sub.6                       
                   3.3     (1H, m) OH                                     
                   5.8     (1H, d) H.sub.3                                
                   6.7     (1H, d) H.sub.2                                
______________________________________                                    
The above results confirm that Compound (I) of this invention had the following formula: ##STR4##
While the invention has been described in detail and with reference to specific embodiments thereof, it will be apparent to one skilled in the art that various changes and modifications can be made therein without departing from the spirit and scope thereof.

Claims (1)

What is claimed is:
1. 4-Hydroxy-4-methyl-cyclohexen-2-one-1 having the formula (I): ##STR5##
US05/932,076 1977-08-08 1978-08-08 4-Hydroxy-4-methyl-cyclohexen-2-one-1 Expired - Lifetime US4250117A (en)

Applications Claiming Priority (2)

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JP52094162A JPS591249B2 (en) 1977-08-08 1977-08-08 4-Hydroxy-4-methyl-cyclohexen-2-one-1
JP52-94162 1977-08-08

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US (1) US4250117A (en)
JP (1) JPS591249B2 (en)
CH (1) CH634812A5 (en)
DE (1) DE2834500C2 (en)
FR (1) FR2399996A1 (en)
GB (1) GB2002373B (en)
IT (1) IT1156895B (en)
NL (1) NL180205C (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4429164A (en) 1981-02-25 1984-01-31 Otsuka Kagaku Yakuhin Kabushini Kaisha Cyclohexadiene derivatives and process for preparing the same
US4871877A (en) * 1988-05-20 1989-10-03 Ethyl Corporation Gem-disubstituted cyclohexadienones and their production
US20060002876A1 (en) * 2004-07-02 2006-01-05 Cahen Christine M Personal care compositions with improved hyposensitivity
US9006169B2 (en) 2005-06-03 2015-04-14 The Procter & Gamble Company Personal care compositions with improved hyposensitivity

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3957887A (en) * 1972-09-18 1976-05-18 Teijin Limited Process for preparing trimethylhydroquinone
US4010205A (en) * 1973-12-07 1977-03-01 Firmenich S.A. Process for the preparation of a diketone derivative
US4076854A (en) * 1977-03-03 1978-02-28 International Flavors & Fragrances Inc. Flavoring with a cyclohexadiene derivative
US4084009A (en) * 1977-03-03 1978-04-11 International Flavors & Fragrances Inc. Flavoring with a hydroxy cyclohexenone derivative

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3957887A (en) * 1972-09-18 1976-05-18 Teijin Limited Process for preparing trimethylhydroquinone
US4010205A (en) * 1973-12-07 1977-03-01 Firmenich S.A. Process for the preparation of a diketone derivative
US4076854A (en) * 1977-03-03 1978-02-28 International Flavors & Fragrances Inc. Flavoring with a cyclohexadiene derivative
US4084009A (en) * 1977-03-03 1978-04-11 International Flavors & Fragrances Inc. Flavoring with a hydroxy cyclohexenone derivative

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Gaoni, "Tetrahedron," vol. 28, pp. 5525-5531, (1972), Pergamon Press. *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4429164A (en) 1981-02-25 1984-01-31 Otsuka Kagaku Yakuhin Kabushini Kaisha Cyclohexadiene derivatives and process for preparing the same
US4871877A (en) * 1988-05-20 1989-10-03 Ethyl Corporation Gem-disubstituted cyclohexadienones and their production
US20060002876A1 (en) * 2004-07-02 2006-01-05 Cahen Christine M Personal care compositions with improved hyposensitivity
WO2006014447A1 (en) * 2004-07-02 2006-02-09 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
EP1666021A1 (en) * 2004-07-02 2006-06-07 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
JP2008505188A (en) * 2004-07-02 2008-02-21 ザ プロクター アンド ギャンブル カンパニー Personal care composition with reduced irritation
AU2005269998B2 (en) * 2004-07-02 2009-01-08 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
US8455417B2 (en) 2004-07-02 2013-06-04 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
US10183051B2 (en) 2004-07-02 2019-01-22 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
US9006169B2 (en) 2005-06-03 2015-04-14 The Procter & Gamble Company Personal care compositions with improved hyposensitivity
US9585866B2 (en) 2005-06-03 2017-03-07 The Procter & Gamble Company Personal care compositions with improved hyposensitivity

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Publication number Publication date
FR2399996B1 (en) 1980-07-18
CH634812A5 (en) 1983-02-28
FR2399996A1 (en) 1979-03-09
NL7808253A (en) 1979-02-12
GB2002373A (en) 1979-02-21
DE2834500C2 (en) 1982-12-30
IT1156895B (en) 1987-02-04
DE2834500A1 (en) 1979-02-22
JPS5430135A (en) 1979-03-06
GB2002373B (en) 1982-01-20
NL180205C (en) 1987-01-16
IT7850633A0 (en) 1978-08-07
NL180205B (en) 1986-08-18
JPS591249B2 (en) 1984-01-11

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